Abstract
Tacrine was the first drug approved by FDA for the treatment of Alzheimer’s disease. However, its use was restricted in function of side effects observed in some patients. Investigations on the structural basis by which tacrine inhibits cholinesterases activity brought new perspectives for the design of more potent analogs with fewer side effects. This review discusses the recent advances on the development of tacrine-structure-based compounds capable to target multiple molecules involved in Alzheimer’s disease. Detailed information on strategies of molecular modifications commonly used in medicinal chemistry, such as bioisosterism, hybridization, dimerization and simplification is presented as well.
Keywords: Alzheimer's disease, tacrine, bioisosterism, dimerization, hybridization, molecular simplification, multi target directed ligands
Current Drug Targets
Title:Design of New Drugs for the Treatment of Alzheimer’s Disease Based on Tacrine Structure
Volume: 14 Issue: 3
Author(s): Roney A.N. de Aquino, Luzia V. Modolo, Rosemeire B. Alves and Angelo de Fatima
Affiliation:
Keywords: Alzheimer's disease, tacrine, bioisosterism, dimerization, hybridization, molecular simplification, multi target directed ligands
Abstract: Tacrine was the first drug approved by FDA for the treatment of Alzheimer’s disease. However, its use was restricted in function of side effects observed in some patients. Investigations on the structural basis by which tacrine inhibits cholinesterases activity brought new perspectives for the design of more potent analogs with fewer side effects. This review discusses the recent advances on the development of tacrine-structure-based compounds capable to target multiple molecules involved in Alzheimer’s disease. Detailed information on strategies of molecular modifications commonly used in medicinal chemistry, such as bioisosterism, hybridization, dimerization and simplification is presented as well.
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Cite this article as:
A.N. de Aquino Roney, V. Modolo Luzia, B. Alves Rosemeire and de Fatima Angelo, Design of New Drugs for the Treatment of Alzheimer’s Disease Based on Tacrine Structure, Current Drug Targets 2013; 14 (3) . https://dx.doi.org/10.2174/1389450111314030010
DOI https://dx.doi.org/10.2174/1389450111314030010 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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